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Thymus tetrapeptide active isomer and its preparation method and medicinal uses

An isomer and thymus technology, which is used in the preparation of immunomodulatory drugs, anti-tumor drugs and anti-oxidant drugs, can solve problems such as unfavorable treatment and short half-life, and achieves improved bioavailability, improved stability, prolonged In vivo half-life effects

Inactive Publication Date: 2007-05-16
JILIN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For healthy individuals, it is normal for peptide hormones to be cleared quickly after they play a regulatory role in the body, but for patients, when drug therapy is required, the short half-life is not good for treatment

Method used

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  • Thymus tetrapeptide active isomer and its preparation method and medicinal uses
  • Thymus tetrapeptide active isomer and its preparation method and medicinal uses
  • Thymus tetrapeptide active isomer and its preparation method and medicinal uses

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0111] Solid Phase Synthesis of LW401

[0112] LW401: Arg-Lys-β-Asp-Val

[0113]

[0114] Raw materials: Fmoc-Val-Wang resin, Fmoc-β-Asp-otBu, Fmoc-Arg(pbf)-OH, Fmoc-Lys(Boc)-OH, coupling reaction condensing agent is benzotriazole-1-oxygen- Tris(dimethylamino)phosphorus hexafluorophosphate (BOP), 1-hydroxybenzotriazole (HOBT), N-methylmorpholine (NMM). The deprotecting agent is 20% piperidine / DMF solution. The cleavage reagent is trifluoroacetic acid.

[0115] Reaction: Weigh Fmoc-Val-Wang resin, swell in DMF at room temperature for 30 minutes, and wash with DMF three times. Add 20% piperidine / DMF solution and react at room temperature for 1 hour to deprotect. Then wash with DMF three times, Fmoc-β-Asp-otBu, react at room temperature for 3 hours, then wash with DMF three times, add 20% piperidine / DMF solution, react at room temperature for 1 hour to deprotect. Then wash with DMF three times, add Fmoc-Lys(Boc)-OH, react at room temperature for 3 hours, then wash with DM...

Embodiment 2

[0119] Solid Phase Synthesis of LW402

[0120] LW402: Arg-β-Lys-Asp-Val

[0121]

[0122] Raw materials: Fmoc-Val-Wang resin, Fmoc AspotBu, Fmoc-Arg(pbf)-OH, Fmoc-β-Lys(Boc)-OH, coupling reaction condensing agent is benzotriazole-1-oxygen-tri( Dimethylamino)phosphorus hexafluorophosphate (BOP), 1-hydroxybenzotriazole (HOBT), N-methylmorpholine (NMM). The deprotecting agent is 20% piperidine / DMF solution. The cleavage reagent is trifluoroacetic acid.

[0123] Reaction: Weigh Fmoc-Val-Wang resin, swell in DMF at room temperature for 30 minutes, and wash with DMF three times. Add 20% piperidine / DMF solution and react at room temperature for 1 hour to deprotect. Then wash with DMF three times, Fmoc-Asp-otBu, react at room temperature for 3 hours, then wash with DMF three times, add 20% piperidine / DMF solution, react at room temperature for 1 hour to deprotect. Then wash with DMF three times, add Fmoc-β-Lys(Boc)-OH, react at room temperature for 3 hours, then wash with DMF ...

Embodiment 3

[0127] Solid Phase Synthesis of LW403

[0128] LW403: Arg-Lys-γ-Glu-Val

[0129]

[0130] Raw materials: Fmoc-Val-Wang resin, Fmoc-Lys-(Boc)-OH, Fmoc-Arg(pbf)-OH, Fmoc-γ-Glu-otBu, coupling reaction condensing agent is benzotriazole-1-oxygen - Tris(dimethylamino)phosphorus hexafluorophosphate (BOP), 1-hydroxybenzotriazole (HOBT), N-methylmorpholine (NMM). The deprotecting agent is 20% piperidine / DMF solution. The cleavage reagent is trifluoroacetic acid.

[0131] Reaction: Weigh Fmoc-Val-Wang resin, swell in DMF at room temperature for 30 minutes, and wash with DMF three times. Add 20% piperidine / DMF solution and react at room temperature for 1 hour to deprotect. Then wash with DMF three times, add Fmoc-γ-Glu-otBu, react at room temperature for 3 hours, then wash with DMF three times, add 20% piperidine / DMF solution, react at room temperature for 1 hour to deprotect. Then wash with DMF three times, add Fmoc-Lys(Boc)-OH, react at room temperature for 3 hours, then wash w...

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PUM

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Abstract

The invention discloses a thymic active isomer and preparing method for industrial manufacturing domain, which possesses amino sequence as X-Arg-Lys-Y-Val, wherein X is acetyl or hydrogen or random sequence with at least 70% isogenesis as the amino sequence; Y is Asp or Glu; Lys or Glu is substituted by corresponding beta-or delta-amino sequence. The invention also provides its medical utility, which can produce immune adjusting drug, tumour-resistance drug and oxidation resistance drug.

Description

technical field [0001] The invention discloses an active isomer of thymosin tetrapeptide and a preparation method thereof, and also discloses its application in preparing immunomodulatory drugs, antitumor drugs and antioxidant drugs, and belongs to the technical field of biopharmaceuticals. Background technique [0002] Current biotechnology has isolated and purified several thymosin peptides from thymus hormones, including thymopoietin II, which consists of 49 amino acid residues, and thymosin α, which consists of 28 amino acid residues. 1 and thymononapeptide etc. Native sequence thymostripeptide (TP-3), tetrapeptide (TP-4) and pentapeptide (TP-5) are residue fragments of thymopoietin II, and it has been reported that they still have thymopoietin activity. [0003] Experiments have shown that thymosin can be partially absorbed in the small intestine and can improve immune function. However, thymopentin is easily hydrolyzed by various enzymes in the body, such as trypsin,...

Claims

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Application Information

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IPC IPC(8): C07K5/023C07K5/027C07K5/037C07K1/04A61K38/07A61P35/00A61P37/02A61P39/06
Inventor 李惟王丽萍王丽凤陈晓光
Owner JILIN UNIV
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